Synthesis and biological evaluation of novel C-aryl d-glucofuranosides as sodium-dependent glucose co-transporter 2 inhibitors

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• 作者：Tzung-Sheng Lin ; Ya-Wen Liw ; Jen-Shin Song ; Tsung-Chih Hsieh ; Hsien-Wei Yeh ; Lih-Ching Hsu ; Chun-Jung Lin ; Szu-Huei Wu ; Pi-Hui Liang
• 关键词：Antidiabetics ; SGLT ; Glucofuranosides
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2013
• 出版时间：1 November, 2013
• 年：2013
• 卷：21
• 期：21
• 页码：6282-6291
• 全文大小：791 K

文摘

Novel C-aryl-d-glucofuranosides were synthesized and evaluated for their capacity to inhibit human sodium-dependent glucose co-transporter 2 (hSGLT2) and hSGLT1. Compound 21q demonstrated the best in vitro inhibitory activity against SGLT2 in this series (EC₅₀ = 0.62 ¦ÌM).